Towards a more selective analogue of oxaliplatin: Synthesis of (Pt((1R,2R)-diaminocyclohexane)(3-carboxypredicentrinato))

A novel oxaliplatin analogue, [Pt((1R,2R)-diaminocyclohexane)(3-carboxypredicentrinato)], boldiplatin, has been synthesized by the coordination of the boldine derivative 3-carboxypredicentrinate to the corresponding platinum(II) moiety in 5.8% overall yield. The complex was fully characterized and biologically evaluated in vitro. Boldiplatin was compared with its parent drug oxaliplatin, showing equal activity over four human tumor cell lines (MCF-7, MDA-MB-231, PC-3 and HT-29) and a tenfold decrease in toxicity over a non-tumor cell line (DHF). This selectivity makes boldiplatin a good candidate for further evaluations to assess its potential as antitumor drug.